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8-Week PK/PD Atorvastatin Study In Children And Adolescents With Heterozygous Familial Hypercholesterolemia

Phase 1
Completed
Conditions
Pediatric Heterozygous Hypercholesterolemia
Interventions
Registration Number
NCT00739999
Lead Sponsor
Pfizer's Upjohn has merged with Mylan to form Viatris Inc.
Brief Summary

To evaluate pharmacokinetics, pharmacodynamics, safety and tolerability of atorvastatin in children and adolescents with heterozygous familial hypercholesterolemia

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
39
Inclusion Criteria
  • Genetically confirmed heterozygous familial hypercholesterolemia (HeFH) with LDL greater or equal 4 mmol/L at baseline
Exclusion Criteria
  • Evidence or history of clinically significant diseases, homozygous familial hypercholesterolemia (FH)

Study & Design

Study Type
INTERVENTIONAL
Study Design
PARALLEL
Arm && Interventions
GroupInterventionDescription
2Atorvastatin10-17 years will be administered 10-mg daily dose of atorvastatin tablet formulation.
1Atorvastatin6-10 years will be administered with atorvastatin tablet formulation with initial doses based on age cohort.
Primary Outcome Measures
NameTimeMethod
Parent-metabolite Population Pharmacokinetic (PK) Model for Atorvastatin and Its Metabolites: Atorvastatin Apparent Clearance (CL/F)Week 2, Week 4, Week 6, Week 8

Parent-metabolite population PK model built using sparse blood samples from both Tanner Stage 1 and Tanner Stage 2+. Blood sampling times: Weeks 2 and 6: single sample between 4 and 12 hours postdose; Weeks 4 and 8: predose, 1 hour, and 2 hours postdose. Plasma samples were analyzed for atorvastatin and active hydroxyacid metabolite (o-hydroxyatorvastatin) concentrations using a validated, sensitive, and specific high-performance liquid chromatography tandem mass spectrometric method. Data presented are the result of the model used.

Parent-metabolite Population Pharmacokinetic (PK) Model for Atorvastatin and Its Metabolites: Apparent Volume of Distribution of the Central Compartment (Vc/F)Week 2, Week 4, Week 6, Week 8

Parent-metabolite population PK model built using sparse blood samples from Tanner Stages 1 and 2+. Sampling times: Weeks 2 + 6: single sample between 4 -12 hours postdose; Weeks 4 + 8: predose, 1 + 2 hours postdose. Plasma samples analyzed for atorvastatin and active hydroxyacid metabolite (o-hydroxyatorvastatin) concentrations using validated, sensitive, specific high-performance liquid chromatography tandem mass spectrometric method. Vc/F value based on 70 kg body weight. Parameter estimation uncertainty (95% CI) by non-parametric bootstrap analysis. Data presented are result of model used.

Secondary Outcome Measures
NameTimeMethod
Absolute Change From Baseline in Pharmacodynamic Responses of Low-density Lipoprotein Cholesterol (LDL-C)Baseline, Week 2, Week 4, Week 6, Week 8

Low-density lipoprotein cholesterol (LDL-C) measured in millimoles per liter (mmol/L); assessments were performed in the fasting state (minimum 10-hour fast \[optional at Weeks 2 and 6\]). Change from baseline = value at observation minus baseline value.

Percent Change From Baseline in Pharmacodynamic Responses of Low-density Lipoprotein Cholesterol (LDL-C)Baseline, Week 2, Week 4, Week 6, Week 8

Low-density Lipoprotein Cholesterol (LDL-C): percent (%) change from baseline by treatment over time = \[LDL-C at observation minus LDL-C at Week 0\] divided by LDL-C at Week 0 \* 100. Assessments were performed in the fasting state (minimum 10-hour fast \[optional at Weeks 2 and 6\]).

Absolute Change From Baseline in Total Cholesterol (TC)Baseline, Week 2, Week 4, Week 6, Week 8

Total Cholesterol measured in millimoles per liter (mmol/L); assessments were performed in the fasting state (minimum 10-hour fast \[optional at Weeks 2 and 6\]). Change from baseline = value at observation minus baseline value.

Percent Change From Baseline in High-Density Lipoprotein Cholesterol (HDL-C)Baseline, Week 2, Week 4, Week 6, Week 8

High-density lipoprotein cholesterol (HDL-C): percent (%) change by treatment over time = \[HDL-C at observation minus HDL-C at Week 0\] divided by HDL-C at Week 0 \* 100. Assessments were performed in the fasting state (minimum 10-hour fast \[optional at Weeks 2 and 6\]).

Absolute Change From Baseline in Apolipoprotein A-1 (Apo A-1)Baseline, Week 2, Week 4, Week 6, Week 8

Change from baseline in Apolipoprotein A-1 measured in grams per liter (g/L); assessments were performed in the fasting state (minimum 10-hour fast \[optional at Weeks 2 and 6\]). Change from baseline = value at observation minus baseline value.

Absolute Change From Baseline in Apolipoprotein B (Apo B)Baseline, Week 2, Week 4, Week 6, Week 8

Change from baseline in Apolipoprotein B measured in grams per liter (g/L); assessments were performed in the fasting state (minimum 10-hour fast \[optional at Weeks 2 and 6\]). Change from baseline = value at observation minus baseline value.

Percent Change From Baseline in Total Cholesterol (TC)Baseline, Week 2, Week 4, Week 6, Week 8

Total cholesterol (TC): percent (%) change from baseline by treatment over time = \[TC at observation minus TC at Week 0\] divided by TC at Week 0 \* 100. Assessments were performed in the fasting state (minimum 10-hour fast \[optional at Weeks 2 and 6\]).

Absolute Change From Baseline in Very Low-density Lipoprotein-cholesterol (VLDL-C)Baseline, Week 2, Week 4, Week 6, Week 8

Change from baseline in very low-density lipoprotein-cholesterol (VLDL-C) measured in millimoles per liter (mmol/L). Change from baseline = value at observation minus baseline value. Assessments were performed in the fasting state (minimum 10-hour fast \[optional at Weeks 2 and 6\]).

Absolute Change From Baseline in Triglycerides (TG)Baseline, Week 2, Week 4, Week 6, Week 8

Change from baseline in triglycerides measured in millimoles per liter (mmol/L); assessments were performed in the fasting state (minimum 10-hour fast \[optional at Weeks 2 and 6\]). Change from baseline = value at observation minus baseline value.

Percent Change From Baseline in Triglycerides (TG)Baseline, Week 2, Week 4, Week 6, Week 8

Triglycerides (TG): percent (%) change from baseline by treatment over time = \[TG at observation minus TG at Week 0\] divided by TG at Week 0 \* 100. Assessments were performed in the fasting state (minimum 10-hour fast \[optional at Weeks 2 and 6\]).

Absolute Change From Baseline in High-Density Lipoprotein Cholesterol (HDL-C)Baseline, Week 2, Week 4, Week 6, Week 8

Change from baseline in high-density lipoprotein cholesterol measured in millimoles per liter (mmol/L); assessments were performed in the fasting state (minimum 10-hour fast \[optional at Weeks 2 and 6\]). Change from baseline = value at observation minus baseline value.

Percent Change From Baseline in Apolipoprotein A-1 (Apo A-1)Baseline, Week 2, Week 4, Week 6, Week 8

Apolipoprotein A-1 (Apo A-1): percent (%) change from baseline by treatment over time = \[Apo A-1 at observation minus Apo A-1 at Week 0\] divided by Apo A-1 at Week 0 \* 100. Assessments were performed in the fasting state (minimum 10-hour fast \[optional at Weeks 2 and 6\]).

Absolute Change From Baseline in Flow-Mediated Dilatation at Week 8Baseline, Week 8

Brachial artery flow-mediated dilatation (FMD) = (max minus baseline diameter divided by baseline diameter) x 100%. Standardized image acquisition: brachial artery images recorded for one minute at rest, blood pressure cuff inflated to 250 mm Hg for 5 minutes with brachial artery imaged continuously throughout cuff inflation, cuff released to produce reactive hyperaemia and the brachial artery imaged continuously for 3 minutes after release. Total duration of measurement approximately 25 minutes. Change from baseline = value at observation minus baseline value.

Percent Change From Baseline in Apolipoprotein B (Apo B)Baseline, Week 2, Week 4, Week 6, Week 8

Apolipoprotein B (Apo B): percent (%) change from baseline by treatment over time = \[Apo B at observation minus Apo B at Week 0\] divided by Apo B at Week 0 \* 100. Assessments were performed in the fasting state (minimum 10-hour fast \[optional at Weeks 2 and 6\]).

Percent Change From Baseline in Very Low-density Lipoprotein-cholesterol (VLDL-C)Baseline, Week 2, Week 4, Week 6, Week 8

Very low-density lipoprotein-cholesterol (VLDL-C): percent (%) change from baseline by treatment over time = \[VLDL-C at observation minus VLDL-C at Week 0\] divided by VLDL-C at Week 0 \* 100. Assessments were performed in the fasting state (minimum 10-hour fast \[optional at Weeks 2 and 6\]).

Percent Change From Baseline in Flow-Mediated Dilatation at Week 8Baseline, Week 8

Brachial Flow-Mediated Dilatation (FMD) = (max minus baseline diameter divided by baseline diameter) x 100%.

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Trial Locations

Locations (1)

Pfizer Investigational Site

🇳🇴

Oslo, Norway

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